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PAR2 mimetic peptides and uses thereof

a technology of mimetic peptides and par2, which is applied in the field of medical pharmacology, can solve the problems of difficult applicability, lack of suitable pharmacological tools, and hinder the full exploration of the role of par2 in disease conditions

Active Publication Date: 2022-06-07
BOARD OF RGT THE UNIV OF TEXAS SYST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is about developing new compounds that can activate or inhibit the PAR2 protein, which is involved in pain and inflammation. The goal is to use these compounds to better understand the role of PAR2 in these conditions and to develop new treatments for them. The invention includes small molecule compounds and peptides that can activate or inhibit PAR2. These compounds can be used to study the function of PAR2 in animals and humans, and may have potential as new analgesics for chronic pain and asthma.

Problems solved by technology

This approach can be problematic, however, because this peptide sequence also activates mas-related G protein-coupled receptors (Mrgpr and GPCRs) that are specifically expressed in the sensory system and are involved in pain and itch signalling (Sci Signal 2011; 4:ra45).
Although PAR2− / − mice have been indispensable for elucidating the role of this receptor in normal physiology and pathology (Physiol Rev 2004; 84:579-621), a lack of suitable pharmacological tools have hindered full exploration of the role of this receptor in disease conditions, including chronic pain (Pharmacol Ther 2011; 130:248-82).

Method used

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  • PAR2 mimetic peptides and uses thereof
  • PAR2 mimetic peptides and uses thereof
  • PAR2 mimetic peptides and uses thereof

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example i

[0134]Protease-activated receptor-2 (PAR2) belongs to a four-member family of G-Protein coupled receptors (GPCRs) that contain internal ligands exposed following exogenous or endogenous protease cleavage of the extracellular amino terminus. PAR2 is associated with a variety of inflammatory conditions, including asthma and pain. The contributions of PAR2 signalling to disease has been hindered by the lack of potent, efficacious antagonists, and their potential for biased-ligand signalling. It was recently demonstrated that lipid tethering of known PAR2 peptidomimetic agonists based on the primary trypsin cleavage sequence (SLIGRL (SEQ ID NO: 19)) increased their potency >200 fold.

[0135]Here, lipid tethering (hexadecyl (Hdc) group with polyethylene glycol (PEG) spacers) and heterocycle (2-aminothiazoyl; 2-at) substitution of hexapeptide sequence derived from the primary cleavage site of kallikreins 4 / 16 (SSKGRS (SEQ ID NO:9)) was used to elucidate novel PAR2 antagonists. Compound 562 ...

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Abstract

This invention is in the field of medicinal pharmacology. In particular, the invention relates to protease activated receptor type 2 (PAR2) modulating compounds (e.g., mimetic peptides), compositions comprising such modulating compounds, and their use as therapeutics for the treatment of conditions involving PAR2 activity.

Description

CROSS REFERENCE TO RELATED APPLICATION[0001]The present application is a U.S. 371 national phase entry of International Patent Application No. PCT / US2017 / 025511, filed Mar. 31, 2017, which claims priority to U.S. Provisional Patent Application Ser. No. 62 / 317,305, filed Apr. 1, 2016, the disclosure of which is herein incorporated by reference in their entireties.STATEMENT REGARDING FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT[0002]This invention was made with government support under Grant No. R01 NS073664 awarded by NIH. The government has certain rights in the invention.INCORPORATION-BY-REFERENCE OF MATERIAL SUBMITTED ELECTRONICALLY[0003]Incorporated by reference in its entirety herein is a computer-readable nucleotide / amino acid sequence listing submitted concurrently herewith and identified as follows: One 3,000 byte ASCII (Text) file named “33999_Replacement_ST25.txt.” created on Aug. 12, 2021.FIELD OF THE INVENTION[0004]This invention is in the field of medicinal pharmacology. ...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K38/08C07K7/00A61K47/60C07K14/705C07K5/083C07K5/10A61K47/61C07K5/103C07K1/22C12N9/76C12N9/64C07K5/117C07K5/062A61K47/62A61K47/54A61K38/17A61K38/00
CPCA61K47/60A61K38/177A61K47/542A61K47/543A61K47/545A61K47/61A61K47/62C07K1/22C07K5/06034C07K5/081C07K5/0808C07K5/10C07K5/101C07K5/1013C07K5/1024C07K14/705C12N9/6427C12N9/6445A61K38/00
Inventor BOITANO, SCOTT A.VAGNER, JOSEFPRICE, THEODORE J.
Owner BOARD OF RGT THE UNIV OF TEXAS SYST
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